曲克芦丁片的人体生物等效性研究

Bioequivalence of Troxerutin Tablets in Healthy Volunteers

目的：研究2种曲克芦丁片的人体相对生物利用度，评价其生物等效性。方法：20名健康男性志愿者按照2制剂2周期的随机交叉试验设计，分别单剂量口服参比制剂和受试制剂，剂量均为900mg，采用液相色谱-串联质谱法测定人血浆中曲克芦丁的浓度，用DAS1．0软件计算各药代动力学参数，并进行生物等效性统计分析。结果：受试制剂和参比制剂的主要药代动力学参数：cmax分别为（1．83±0．90）和（2．02±1．54）ng／ml；tmax分别为（1．20±0．50）和（1．00±0．40）h；AUC0-12h分别为（8．48±3．74）和（8．51±5．44）ng·h·ml^-1；AUC0-∞。分别为（9．47±4．55）和（9．97±6．15）ng·h·ml^-1；t1／2分别为（2．80±2．00）和（4．00±2．40）h。2种制剂的cmax、tmax、AUC0-12b和AUC0-∞均无显著性差异，双单侧t检验结果表明，受试制剂cmax的90％置信区间落在参比制剂的70％-143％范围内，受试制剂AUC的90％置信区间均落在参比制剂的80％-125％范围内，受试制剂的相对生物利用度为（113．6±39．5）％。结论：曲克芦丁片2种剂具有生物等效性。

Objective ：To evaluate the relative bioavailahility and bioequivalence of two kinds of troxerutin tablets in heahhy male volunteers. Methods：In a randomized crossover design ,20 healthy male volunteers were given a single oral dose of 900 mg test or reference troxerutin tablets. The concentrations of troxerutin in human plasma were determined by a HPLC-MS/MS method. Results：The main pharmacokinetic parameters of the test and reference troxerutin tablets were as follows ：cmax were （ 1.83 ± 0.90） and （2.02 ± 1.54） ng/ml, tmax were （ 1.2 ± 0.5） and （1.0±0.4） h,AUC0-12h were （8.48 ±3.47） and （8.51 ±5.44） ng·h· ml^-1,AUC0-∞ were （9.47 ± 4.55） and （9.97 ±6. 15 ） ng·h · ml^-1 ,and t1/2 were （2.8 ± 2.0） and （4.0 ± 2.4） h,respectively. The relative bioavailability of the test tablets was （ 113.6 ± 39.5 ） %. There was no significant difference in cmax, tmax AUC0 - 12h and AUC0 - ∞ between the two preparations. 90% of the confidential interval of cmax and AUC were between 70% ± 143% ,and 80% ± 125% respectively according to those of reference tablets. Conclusion：The two preparations were bioequivalent.